INESTOM 1g / 10ml № 10

Inestom


International nonproprietary name

Levocarnitine


Dosage form

Oral solution, 1 g/10 ml

Compound

1 ml of the drug contains

active substance - levocarnitine 100.0 mg,

Excipients: malic acid, methylparaben (E 218), propylparaben (E 216), sodium saccharin dihydrate, orange flavor, purified water.

Description

Transparent solution from colorless to yellowish.




Pharmacotherapeutic group

Other drugs for the treatment of gastrointestinal diseases and metabolic disorders. Amino acids and their derivatives. Levocarnitine.

ATX code A16AA01

Pharmacological properties

Pharmacokinetics

After ingestion, levocarnitine (L-carnitine), as a result of the action of intestinal flora, is metabolized into trimethylamine 
(TMA) and γ-butyrobetaine. Approximately 10-20% of levocarnitine reaches the systemic circulation unchanged. Therefore,
it is believed that intestinal metabolism is responsible for the elimination of 80-90% of an orally administered dose.
Both metabolites, TMA and γ-butyrobetaine, are absorbed in the small intestine. γ-butyrobetaine is excreted unchanged in urine,
while TMA is metabolized in the liver to trimethylamine-N-oxide (TMAO) and is found in urine, mainly as TMAO, with small amounts as unchanged TMA.

In cases of hemocatharsis (blood purification), end-stage renal failure or chronic use of levocarnitine,
the amount of TMA and TMAO in the blood increases and, as a consequence, the amount of TMA in the urine increases.


Levocarnitine, after absorption through the intestines, reaches its maximum concentration in the blood after 3 hours. 
High levels of levocarnitine are maintained in the blood plasma for 9 hours. Excreted by the kidneys, 
more than 80% of the dose taken remains unchanged within 24 hours. Levocarnitine can be found in muscles and organ parenchyma.

Pharmacodynamics

Levocarnitine is present as a natural component in the tissues of animals, microorganisms and plants.
In the human body, the requirements for normal metabolism are met through the consumption of foods containing carnitine,
as well as through endogenous synthesis in the liver and kidneys from lysine and methionine, which are donors of the methyl group. 
Only the L-isomer of carnitine (levocarnitine) is biologically active and plays a major role in lipid metabolism, 

In the metabolism of ketone bodies, as a link in the amino acid chain.

Levocarnitine is involved in the transport of long-chain fatty acids in mitochondria
(promotes the oxidation of fatty acids), that is, it participates as a carrier of fatty acids
across cell membranes from the cytoplasm to the mitochondria, where it undergoes the process
of beta-oxidation with the formation of a large amount of metabolic energy in the form of ATP.
Левокарнитин улучшает работу цикла Кребса (путем освобождения СоА, действия СоА, при участии фермента  карнитин-ацилтрансферазы), 
стимулирует активность пируват дегидрогеназы в скелетных мышцах и окисление разветвленных звеньев цепи аминокислот.
Таким образом, левокарнитин прямо или косвенно включается в различные процессы обмена веществ и является важным фактором
не только окисления жирных кислот и кетоновых тел, но также глюкозы и некоторых аминокислот.

Indications for use

- primary and secondary levocarnitine deficiency in adults and children over 12 years of age

Directions for use and doses

The drug is taken orally, the solution can be drunk without dilution or diluted in 100 ml of chilled boiled water or fruit juice.

To determine the optimal dose, it is recommended to monitor therapy by measuring the levels of free
and acyl levocarnitine in blood plasma and urine. The level of free levocarnitine in the blood plasma should be 35 - 60 mol/l.
The ratio of acyl levocarnitine to the level of free levocarnitine in blood plasma should not be higher than 0.35.

Adults and children over 12 years old

Primary and   secondary levocarnitine deficiency: recommended doses

Inestomas depend on the metabolic disorder and the severity during the treatment period. 
In most cases, the recommended oral dose is 100-200 mg/kg/day in 2-4 divided doses. 
If clinical and biochemical parameters do not improve, the dose may be increased for a short time. High doses up to 400 mg/kg/day may be necessary for acute metabolic decompensation

In case of secondary carnitine deficiency in patients with end-stage chronic renal failure receiving hemodialysis: 
if significant clinical improvement was achieved after the first course of intravenous use of Inest,
maintenance therapy with Inest, oral solution, is prescribed at a dose of 1 g/day.

Side effects

Side effects are not observed when using Inest, as prescribed by the doctor.

Rarely

- nausea, vomiting, abdominal pain, diarrhea

Reducing the dose leads to elimination of side effects.

- muscle weakness, cramps in patients with uremia

- allergic reactions (skin itching, skin rash, urticaria, Quincke's edema, anaphylactic shock)

- specific body odor

- increase in INR (International Normalized Ratio) when used together with coumarins (acenocoumarol or warfarin)

Contraindications

- hypersensitivity to the components of the drug

- children's age up to 12 years


Drug interactions

Prescribing Inestoma to patients with diabetes mellitus receiving insulin or oral hypoglycemic drugs may cause hypoglycemia due to increased glucose absorption. 
Therefore, in this category of patients, during treatment with Inest, 
the level of glucose in the blood plasma should be constantly monitored to correct the dosage regimen of hypoglycemic drugs.

Glucocorticosteroids contribute to the accumulation of the drug in tissues (except the liver).

Lipoic acid and anabolic steroids enhance the effect of levocarnitine.

There have been very rare reports of increased INR in patients receiving coumarin anticoagulants together with levocarnitine. 
Patients receiving such anticoagulants concomitantly with levocarnitine should have their 
INR or other appropriate coagulation test monitored weekly until stabilized and monthly thereafter.

If you use any other medications together with Inestom, you must inform your doctor about this.

Special instructions

Inestome is not addictive or addictive because it is a natural component of the body.

Tolerance to the drug should be monitored during the first week of treatment and after each dose increase.

Ingestion of high doses of Inestoma is not recommended for patients with severely impaired renal function or those on dialysis in end-stage renal disease, this may lead to the accumulation of potentially toxic metabolites trimethylamine (TMA) and trimethyl-N-oxide (TMAO), which are usually excreted in the urine . This can cause a "fishy odor" in urine, breath and sweat. This situation is not observed after intravenous administration of levocarnitine.

The drug is used with caution in patients with a history of allergic reactions, chronic heart failure, acute renal failure, 
edema caused by salt retention, as well as patients taking corticosteroid and corticotropic hormonal drugs. 
Long-term use of the drug without additional potassium intake may lead to hypokalemia.

Inestom, oral solution, contains propylparaben and methylparaben, which may cause allergic reactions (possibly delayed).

Use during pregnancy and lactation

Due to the lack of research, use during pregnancy and lactation is not recommended.

Features of the influence on the ability to drive a vehicle and potentially dangerous mechanisms

Does not affect.

Overdose

Symptoms: Large doses of levocarnitine can cause diarrhea.

Treatment: if necessary - symptomatic therapy.

Release form and packaging

10 ml of the drug in a flint glass bottle with a tightly screwed polyethylene cap.

A label made of label paper is attached to each bottle.

10 bottles each along with instructions for medical use in the state and Russian languages ​​are placed in a cardboard box.

Storage conditions

In a place protected from light, at a temperature no higher than 25 ºС.

Keep out of the reach of children!

Shelf life

3 years

Do not use the drug after the expiration date indicated on the package.




Conditions for dispensing from pharmacies

On prescription

Manufacturer

Help S.A., 10 Valaoritou Street, 144 52, Athens, Greece

Phone +30 210 281 5353, fax +30 210 281 1850




Registration Certificate Holder

Help S.A.,   Athens, Greece